Drug reference
(meth-ill-fen′i-date) Adhansia XR, Aptensio XR, Biphentin , Concerta, Cotempla XR-ODT, Daytrana, Foquest , Jornay PM, Quillivant XR, Ritalin, Ritalin LA, Ritalin SR , QuilliChew ER, Relexxii
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Func. class.: Cerebral stimulant
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Chem. class.: Piperidine derivative Controlled Substance Schedule II
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Do not confuse: methylphenidate/methadone Ritalin/ritodrine/Ritalin LA
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ACTION: Increases release of norepi- nephrine, DOPamine in cerebral cortex to reticular activating system; exact action not known
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USES: Attention deficit disorder (ADD), attention-deficit/hyperactivity disorder (ADHD); narcolepsy (except Concerta, Metadate CD, Ritalin LA)
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Unlabeled uses: Depression refractory to other therapies
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CONTRAINDICATIONS: Hyper- sensitivity, anxiety, history of Gilles de la Tourette’s syndrome; glaucoma, heredi- tary fructose intolerance Precautions: Pregnancy, breastfeeding, hypertension, depression, seizures, abrupt discontinuation, acute MI, aortic stenosis, arteriosclerosis, bipolar disorder, cardiac dysrhythmias, cardiomyopathy, chemical leukoderma, child depression, dysphagia, esophageal stricture, growth inhibition, heart failure, hepatic disease, hypertension, hyperthyroidism, ileus, mania, peripheral vascular disease, PKU, psychosis, Raynaud’s disease, schizophrenia, stroke, suicidal ide- ation, visual disturbances
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Black Box Warning: Substance abuse, alcoholism Black Box Warning: Substance abuse: there is a high potential for abuse; use caution in those with history of substance abuse • VS, B/P; may reverse antihyperten- sives; check patients with cardiac disease more often for increased B/P • CBC with differential, platelets, LFTs, urinalysis; in diabetes: blood glucose, urine glucose; insulin changes may have to be made because eating will decrease • Height, growth rate q3mo in children; growth rate may be decreased, but nor- mal growth will resume when product is discontinued • Mental status: mood, sensorium, af- fect, stimulation, insomnia, aggres- siveness; may produce euphoria, re- bound depression after product wears off • Withdrawal symptoms: headache, nausea, vomiting, muscle pain, weakness; usually not associated with drug holidays • Appetite, sleep, speech patterns • Narcolepsy: identify frequency, length of narcoleptic episodes • Skin pigmentation when using TD product; may cause loss of pigmentation around site • Beers: avoid use in older adults; CNS stimulant effects • Pregnancy/breastfeeding: use only if benefit outweighs risk to fetus; no well- controlled studies; cautious use in breastfeeding
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SIDE EFFECTS CNS: Hyperactivity, insomnia, restless- ness, talkativeness, dizziness, drowsi- ness, toxic psychosis, headache, akathi- sia, dyskinesia, masking or worsening of Tourette’s syndrome, seizures, hallucina- tions, malignant neuroleptic syndrome, aggression; cerebral vasculitis, hemor- rhage, stroke (rare) CV: Palpitations, tachycardia, B/P changes, angina, dysrhythmias, sudden death ENDO: Growth retardation GI: Nausea, anorexia, dry mouth, weight loss, abdominal pain HEMA: Leukopenia, anemia, thrombocy- topenic purpura INTEG: Exfoliative dermatitis, urticaria, rash, erythema multiforme, hypersensi- tivity reactions; patch: permanent loss of skin color, anaphylaxis, angioedema MISC: Fever, arthralgia, scalp hair loss, rhabdomyolysis
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INTERACTIONS Increase: hypertensive crisis—MAOIs or within 14 days of MAOIs, vasopressors Increase: effects of tricyclics, SSRIs, anti- convulsants, SNRIs, CNS stimulants; monitor for adverse reactions Decrease: effect of antihypertensives Drug/Herb Increase: CNS stimulation—cola nut, guarana, horsetail, yerba maté, yohimbe Drug/Food Increase: stimulation—caffeine
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TREATMENT OF OVERDOSE: Administer fluids; hemodialysis or peri- toneal dialysis; antihypertensive for M increased B/P; administer short-acting barbiturate before lavage
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DOSAGE AND ROUTES Attention-deficit/hyperactivity dis- order (ADHD) initial treatment, not currently on methylphenidate Regular release: Ritalin • Adult: PO 20-30 mg/day, range 10-60 mg/day in 2-3 divided doses, 30-45 min before meals • Child ≥6 yr: PO 5 mg bid initially, in- crease 5-10 mg/day weekly, usual dose 0.3-2 mg/kg/day, max 60 mg/day Extended-release once-daily tabs: Concerta • Adult: PO 18-36 mg/day initially, then adjust by 18 mg/wk, max 72 mg/day • Adolescent: PO 18 mg/day initially, then adjust by 18 mg/wk, max 72 mg/ day • Child ≥6 yr: PO 18 mg/day initially, then adjust by 18 mg/wk, max 54 mg/day Extended-release once-daily capsules: Ritalin LA • Adult/adolescent/child ≥6 yr: PO 10- 20 mg daily in AM initially, adjust by 10 mg/wk, max 60 mg/day Extended release once-daily PM capsule: • Child >6 yr and adolescents: PO 20 mg in evening; may increase weekly by 20 mg, max 100 mg/day Transdermal: Daytrana • Adolescent/child ≥6 yr: TD wk 1: 10 mg/day (9-hr patch); wk 2: 15 mg/ day (9-hr patch); wk 3: 20 mg/day (9-hr patch); wk 4: 30 mg/day (9-hr patch) Conversion to once-daily treatment from other forms for ADHD Extended-release once-daily cap- sules: Ritalin LA • Adult/adolescent/child ≥6 yr: PO give no more than total daily dose of other forms, may adjust by 10 mg/wk, max 60 mg/day Extended-release once-daily tablets: Concerta • Adult/adolescent/child ≥6 yr (currently on 10-15 mg/day): PO 18 mg every AM initially, adjust by 18 mg/wk, max 72 mg/ day (adult); max 72 mg/day, 2 mg/kg/day (adolescent); 54 mg/day (child) • Adult/adolescent/child ≥6 yr (currently receiving 20-30 mg/day): PO 36 mg every AM, adjust by 18 mg/wk, max 72 mg/day (adult); 72 mg/day, 2 mg/kg/day (adoles- cent); 54 mg/day (child) • Adult/adolescent/child ≥6 yr (currently receiving 30-45 mg/day): PO 54 mg every AM, adjust by 18 mg/wk, max 72 mg/day (adult); 72 mg/day, 2 mg/kg/day (adoles- cent); 54 mg/day (child) • Adult/adolescent/child ≥6 yr (currently receiving 40-60 mg/day): PO 72 mg every AM, 72 mg/day Extended-release once-daily sus- pension: Quillivant XR • Adolescent/child ≥6 yr: PO give 20 mg in AM, increase in 10-20 mg increments weekly Narcolepsy Immediate release: Ritalin • Adult: PO 20-30 mg/day, range 10-60 mg/day in 2-3 divided doses • Child ≥6 yr: PO 5 mg bid, may increase by 5-10 mg/wk, max 60 mg/day
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Available forms: Tabs 5, 10, 20 mg; ext rel tabs 10, 20 mg; ext rel tabs (Con- certa) 18, 27, 36, 54 mg; ext rel caps 10, 20, 30, 40 mg; ext rel chewable tabs (QuillChew ER) 20, 30, 40 mg; oral sol 5 mg/5 mL, 10 mg/5 mL; chew tabs (Methylin) 2.5, 5, 10 mg; transdermal patch 12.5 cm2 (10 mg), 18.75 cm2 (15 mg), 25 cm2 (20 mg), 37.5 cm2 (30 mg); ext rel oral susp 300 mg/60 mL, 600 mg/120 mL, 750 mg/150 mL, 900 mg/180 mL; capsule (Journay PM) 20 mg
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Administer: PO route • Chewable tablets: give with at least 8 oz of fluid to avoid choking • Immediate-release dosage forms (Ritalin, give 30-45 min before meal; twice-daily dosages may be used in AM and noon • Ext-rel tablets: may be given without regard to meals. Give whole; do not cut, crush, or chew. Give the last dose of the day several hours before bedtime. Ext-rel tablets may be used when the determined 8-hr dose of immediate-release methyl- phenidate tablets equals the 8-hr dosage of the ext-rel tablets • Once-daily ext-rel tablets (Concerta): may be given without regard to meals. Give whole; do not cut, crush, or chew; portion of this tablet may appear intact in the stool • Once-daily ext-rel capsules (Ritalin LA, Aptensio XR): may be given without regard to meals; establish a routine pat- tern with regard to meals. Give with an adequate amount of fluid. Do not cut, crush, or chew. If swallowing is difficult, capsule may be opened and the contents sprinkled on 1 tablespoon of applesauce and swallowed immediately. The capsule contents (beads) should not be crushed or chewed. Instruct patient to drink flu- ids (water, milk, or juice) after taking sprinkles with applesauce M • Once-daily ext-rel chewable tablets (QuilliChew ER): give daily in the AM with or without food. The tablet may be bro- ken in half for 10-mg and 15-mg doses • Immediate-release oral solution (Methylin): measure dose with oral sy- ringe or calibrated measuring device. Give 30-45 min before meals in divided doses 2 to 3 times/day. Twice-daily dosages may be administered in AM and around noon. Give last dose of day before 6 PM • Once-daily ext-rel oral suspension (Quillivant XR): vigorously shake before use; measure dose with calibrated oral dosing dispenser provided. Give in AM without regard to meals • Reconstitution of once-daily ext-rel oral suspension (Quillivant XR): review manufacturer’s instructions; before re- constitution, tap bottle to loosen pow- der. Add specified amount of water to bottle, fully insert the bottle adapter into the bottle neck, replace the cap, and vigorously shake for at least 10 sec. Store reconstituted suspension at 77°F; dispense in original packaging (bottle in container). Reconstituted suspension is stable for 4 mo from date of reconsti- tution Topical route • Daytrana transdermal system: apply patch 2 hr before effect is needed • Do not cut or trim patch • Apply patch immediately after open- ing. Do not use if pouch seal is broken. Do not touch adhesive side of patch dur- ing application to avoid absorption. Wash hands immediately if adhesive side of patch is touched. Discard patch if diffi- culty is encountered in separating patch from the release liner, or if tearing or other damage occurs. Discard patch if adhesive containing medication has transferred to the liner during removal of patch from the liner • Place on a dry, clean area of the hip, and hold in place for 30 sec with palm of hand. Do not apply to oily, damaged, or irritated skin. Do not apply topical prep- arations to the application site immedi- ately before patch application. Avoid waistline area where patch could be rubbed by clothing • Application sites should be alternated from one hip to the next each day • Adherence of patch may be affected by showering, bathing, or swimming • Avoid exposing the application site to hair dryers, heating pads, electric blan- kets, heated water beds, or other direct external heat sources • Do not apply or reapply the patch with dressings, tape, or adhesives. If the patch is not fully adhered to the skin during application or wear time, discard patch according to disposal instructions, and apply a new patch • Total daily wear time should not exceed 9 hr, regardless of patch replacement • Patches should be peeled off slowly. Patch removal may be aided by applying an oil-based product (petroleum jelly, mineral oil, olive oil) to the patch edges • For disposal, instruct patient and/or caregiver to fold used patch so that the adhesive side of the patch adheres to it- self, and then flush it down the toilet or dispose of in an appropriate lidded con- tainer
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Assess: • ADHD: attention span, decreased hy- peractivity, impulsivity, socialization
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Evaluate: • Therapeutic response: decreased hy- peractivity (ADHD); increased ability to stay awake (narcolepsy)
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To decrease caffeine consumption (coffee, tea, cola, chocolate); may in- crease irritability, stimulation; not to use guarana, yerba maté, cola nut • To avoid OTC preparations unless ap- proved by prescriber • To always use dosing dispenser pro- vided for oral suspension dose • To taper off product over several weeks because depression, increased sleeping, lethargy will occur • To avoid driving, hazardous activities if dizziness, blurred vision occur • To avoid alcohol • To get needed rest; patients will feel more tired at end of day • That shell of Concerta tab may appear in stools • To take regular tab at least 6 hr before sleep, 10 hr for ext rel; to use dosing sy- ringe, not household teaspoon, to mea- sure liquid • Seizures: that those with seizure disor- ders may have lower seizure threshold • Transdermal: to use in AM; after tray is opened, to use within 2 mo; not to store patches without protective cover- ing; to notify prescriber if skin irritation or rash occurs; that if patch comes off, to use a new one on a different skin site; to tell child not to remove or share with others • Sus rel: not to chew tabs
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PHARMACOKINETICS PO: Varies with formulation, metabolized by liver, excreted by kidneys, half-life 3-4 hr
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• Adolescent: PO 18 mg/day initially, then adjust by 18 mg/wk, max 72 mg/ day
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• Adult/adolescent/child ≥6 yr: PO 10- 20 mg daily in AM initially, adjust by 10 mg/wk, max 60 mg/day Extended release once-daily PM capsule:
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• Child >6 yr and adolescents: PO 20 mg in evening; may increase weekly by 20 mg, max 100 mg/day Transdermal: Daytrana
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• Adolescent/child ≥6 yr: TD wk 1: 10 mg/day (9-hr patch); wk 2: 15 mg/ day (9-hr patch); wk 3: 20 mg/day (9-hr patch); wk 4: 30 mg/day (9-hr patch) Conversion to once-daily treatment from other forms for ADHD Extended-release once-daily cap- sules: Ritalin LA
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• Adult/adolescent/child ≥6 yr: PO give no more than total daily dose of other forms, may adjust by 10 mg/wk, max 60 mg/day Extended-release once-daily tablets: Concerta
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• Adult/adolescent/child ≥6 yr (currently on 10-15 mg/day): PO 18 mg every AM initially, adjust by 18 mg/wk, max 72 mg/ day (adult); max 72 mg/day, 2 mg/kg/day (adolescent); 54 mg/day (child)
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• Adult/adolescent/child ≥6 yr (currently receiving 20-30 mg/day): PO 36 mg every AM, adjust by 18 mg/wk, max 72 mg/day (adult); 72 mg/day, 2 mg/kg/day (adoles- cent); 54 mg/day (child)
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• Adult/adolescent/child ≥6 yr (currently receiving 30-45 mg/day): PO 54 mg every AM, adjust by 18 mg/wk, max 72 mg/day (adult); 72 mg/day, 2 mg/kg/day (adoles- cent); 54 mg/day (child)
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• Adult/adolescent/child ≥6 yr (currently receiving 40-60 mg/day): PO 72 mg every AM, 72 mg/day Extended-release once-daily sus- pension: Quillivant XR
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• Adolescent/child ≥6 yr: PO give 20 mg in AM, increase in 10-20 mg increments weekly Narcolepsy Immediate release: Ritalin
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